Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary for 2.3.3.8 extracted from

  • Feng, X.; Zhang, L.; Xu, S.; Shen, A.Z.
    ATP-citrate lyase (ACLY) in lipid metabolism and atherosclerosis An updated review (2020), Prog. Lipid Res., 77, 101006 .
    View publication on PubMed

Application

Application Comment Organism
drug development Mendelian randomization of large human cohorts has validated ACLY as a promising target for low-density-lipoprotein-cholesterol lowering and cardiovascular protection Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
bempedoic acid i.e. ETC-1002 is a first-in-class, prodrug-based direct competitive inhibitor of ATP citrate lyase which regulates lipid metabolism by upregulating hepatic LDL receptor (LDLr) expression and activity. Pharmacological inhibition of ACLY by bempedoic acid, prevents dyslipidemia and attenuates atherosclerosis in hypercholesterolemic ApoE-/- mice, LDLr-/- mice, and LDLr-/- miniature pigs Homo sapiens
SB-204990 in addition to lowering lipids by inhibiting ACLY, the chemical inhibitor SB-204990 also displays tumor suppressive effects Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
ATP + citrate + CoA Homo sapiens ATP citrate lyase is an important enzyme linking carbohydrate to lipid metabolism by generating acetyl-CoA from citrate for fatty acid and cholesterol biosynthesis ADP + phosphate + acetyl-CoA + oxaloacetate
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens P53396
-
-

Source Tissue

Source Tissue Comment Organism Textmining
hepatocyte ACLY deficiency in hepatocytes protects from hepatic steatosis and dyslipidemia Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + citrate + CoA
-
Homo sapiens ADP + phosphate + acetyl-CoA + oxaloacetate
-
?
ATP + citrate + CoA ATP citrate lyase is an important enzyme linking carbohydrate to lipid metabolism by generating acetyl-CoA from citrate for fatty acid and cholesterol biosynthesis Homo sapiens ADP + phosphate + acetyl-CoA + oxaloacetate
-
?

Synonyms

Synonyms Comment Organism
ACLY
-
Homo sapiens
ATP-citrate lyase
-
Homo sapiens

General Information

General Information Comment Organism
metabolism ATP citrate lyase is an important enzyme linking carbohydrate to lipid metabolism by generating acetyl-CoA from citrate for fatty acid and cholesterol biosynthesis Homo sapiens